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Utility of novel 2-furanones in synthesis of other heterocyclic compounds having anti-inflammatory activity with dual COX2/LOX inhibition
Inflammation is associated with the development of several diseases comprising cancer and cardiovascular disease. Agents that suppress cyclooxygenase (COX) and lipoxygenase (LOX) enzymes, besides chemokines have been suggested to minimise inflammation. Here, a variety of novel heterocyclic and non-h...
Autores principales: | , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Taylor & Francis
2021
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8118430/ https://www.ncbi.nlm.nih.gov/pubmed/33957835 http://dx.doi.org/10.1080/14756366.2021.1908277 |
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author | Abd El-Hameed, Rania H. Mahgoub, Shahenda El-Shanbaky, Hend M. Mohamed, Mosaad S. Ali, Sahar A. |
author_facet | Abd El-Hameed, Rania H. Mahgoub, Shahenda El-Shanbaky, Hend M. Mohamed, Mosaad S. Ali, Sahar A. |
author_sort | Abd El-Hameed, Rania H. |
collection | PubMed |
description | Inflammation is associated with the development of several diseases comprising cancer and cardiovascular disease. Agents that suppress cyclooxygenase (COX) and lipoxygenase (LOX) enzymes, besides chemokines have been suggested to minimise inflammation. Here, a variety of novel heterocyclic and non-heterocyclic compounds were prepared from novel three furanone derivatives. The structures of all synthesised compounds were confirmed by elemental and spectral analysis including mass, IR, and (1)H-NMR spectroscopy. Anti-inflammatory activities of these synthesised compounds were examined in vitro against COX enzymes, 15-LOX, and tumour necrosis factor-α (TNF-α), using inhibition screening assays. The majority of these derivatives showed significant to high activities, with three pyridazinone derivatives (5b, 8b, and 8c) being the most promising anti-inflammatory agents with dual COX-2/15-LOX inhibition activities along with high TNF-α inhibition activity. |
format | Online Article Text |
id | pubmed-8118430 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2021 |
publisher | Taylor & Francis |
record_format | MEDLINE/PubMed |
spelling | pubmed-81184302021-05-21 Utility of novel 2-furanones in synthesis of other heterocyclic compounds having anti-inflammatory activity with dual COX2/LOX inhibition Abd El-Hameed, Rania H. Mahgoub, Shahenda El-Shanbaky, Hend M. Mohamed, Mosaad S. Ali, Sahar A. J Enzyme Inhib Med Chem Research Paper Inflammation is associated with the development of several diseases comprising cancer and cardiovascular disease. Agents that suppress cyclooxygenase (COX) and lipoxygenase (LOX) enzymes, besides chemokines have been suggested to minimise inflammation. Here, a variety of novel heterocyclic and non-heterocyclic compounds were prepared from novel three furanone derivatives. The structures of all synthesised compounds were confirmed by elemental and spectral analysis including mass, IR, and (1)H-NMR spectroscopy. Anti-inflammatory activities of these synthesised compounds were examined in vitro against COX enzymes, 15-LOX, and tumour necrosis factor-α (TNF-α), using inhibition screening assays. The majority of these derivatives showed significant to high activities, with three pyridazinone derivatives (5b, 8b, and 8c) being the most promising anti-inflammatory agents with dual COX-2/15-LOX inhibition activities along with high TNF-α inhibition activity. Taylor & Francis 2021-05-06 /pmc/articles/PMC8118430/ /pubmed/33957835 http://dx.doi.org/10.1080/14756366.2021.1908277 Text en © 2021 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group. https://creativecommons.org/licenses/by/4.0/This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0/ (https://creativecommons.org/licenses/by/4.0/) ), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. |
spellingShingle | Research Paper Abd El-Hameed, Rania H. Mahgoub, Shahenda El-Shanbaky, Hend M. Mohamed, Mosaad S. Ali, Sahar A. Utility of novel 2-furanones in synthesis of other heterocyclic compounds having anti-inflammatory activity with dual COX2/LOX inhibition |
title | Utility of novel 2-furanones in synthesis of other heterocyclic compounds having anti-inflammatory activity with dual COX2/LOX inhibition |
title_full | Utility of novel 2-furanones in synthesis of other heterocyclic compounds having anti-inflammatory activity with dual COX2/LOX inhibition |
title_fullStr | Utility of novel 2-furanones in synthesis of other heterocyclic compounds having anti-inflammatory activity with dual COX2/LOX inhibition |
title_full_unstemmed | Utility of novel 2-furanones in synthesis of other heterocyclic compounds having anti-inflammatory activity with dual COX2/LOX inhibition |
title_short | Utility of novel 2-furanones in synthesis of other heterocyclic compounds having anti-inflammatory activity with dual COX2/LOX inhibition |
title_sort | utility of novel 2-furanones in synthesis of other heterocyclic compounds having anti-inflammatory activity with dual cox2/lox inhibition |
topic | Research Paper |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8118430/ https://www.ncbi.nlm.nih.gov/pubmed/33957835 http://dx.doi.org/10.1080/14756366.2021.1908277 |
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